Fig. 6 | Signal Transduction and Targeted Therapy

Fig. 6

From: Epigenetic drug library screening identified an LSD1 inhibitor to target UTX-deficient cells for differentiation therapy

Fig. 6

SP2509 inhibited Utx-mutated AML by promoting differentiation in vitro and in vivo. a Flow cytometry measuring protein expression in Utx−/−; shp53-mCherry;shNf1-GFP AML cells treated with vehicle or SP2509. Left, representative flow plots of AML cells showing the expression of Mac-1. Right, percentage of Mac-1+ populations (top), and the MFI of Mac-1 staining (bottom). b MFI of cKit staining in AML cells treated with vehicle or SP2509. c Relative cell number of AML cells treated with vehicle or SP2509. d Schematic showing Utx−/−; shp53-mCherry;shNf1-GFP mice with AML treated with vehicle or SP2509. C57BL/6 mice were sublethally irradiated and then transplanted with Utx−/−; shp53-mCherry; shNf1-GFP AML cells. Once AML was established, these mice were treated with vehicle or 25 mg/kg SP2509 twice per week via i.p. injection. The mice were monitored by flow cytometry, CBC, and blood smear. e, f Representative flow plots showing the expression of Mac-1 in peripheral blood AML cells in vehicle- or SP2509-treated mice after 1 (e) or 2 (f) weeks. g, h Percentage of Mac-1+ (g) and MFI of Mac-1 staining (h) of AML cells in the peripheral blood of vehicle- or SP2509-treated mice. i Tumor burden in the peripheral blood of vehicle- or SP2509-treated mice, measured by the percentage of GFP+mCherry+ populations. j Whole blood cell counts in vehicle- or SP2509-treated mice after 2.5 weeks. k Kaplan–Meier survival curves of mice with AML treated with vehicle or SP2509. n = 6, **p < 0.01. l Blood smear showing leukemic cells in the peripheral blood of vehicle- or SP2509-treated mice

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